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首页> 外文期刊>Journal of Medicinal Chemistry >Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2
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Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

机译：4-Oxo-1-芳基-1,4-二氢喹啉-3-羧酰胺作为代谢型谷氨酸受体亚型2的选择性负变构调节剂的设计

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Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu(2/3) inhibition and a variety of CNS diseases and disorders. Though these tools typically have good selectivity for mGlu(2/3) versus the remaining six members of the mGlu family, compounds that are selective for only one of the individual group II mGlus have proved elusive. Herein we report on the discovery of a potent and highly selective mGlu2 negative allosteric modulator 58 (VU6001192) from a series of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides. The concept for the design of this series centered on morphing a quinoline series recently disclosed in the patent literature into a chemotype previously used for the preparation of muscarinic acetylcholine receptor subtype 1 positive allosteric modulators. Compound 58 exhibits a favorable profile and will be a useful tool for understanding the biological implications of selective inhibition of mGlu2 in the CNS.
机译：II组代谢型谷氨酸受体（mGlus）的正构和变构拮抗剂都已被用来建立mGlu（2/3）抑制与多种中枢神经系统疾病和病症之间的联系。尽管与mGlu家族的其余六个成员相比，这些工具通常对mGlu（2/3）具有良好的选择性，但事实证明，仅对单个II类mGlus之一具有选择性的化合物。在本文中，我们报道了从一系列4-氧代-1-芳基-1,4-二氢喹啉-3-羧酰胺中发现的有效且高度选择性的mGlu2负变构调节剂58（VU6001192）。该系列的设计思想集中在将专利文献中最近公开的喹啉系列转变为先前用于制备毒蕈碱型乙酰胆碱受体亚型1阳性变构调节剂的化学型。化合物58表现出良好的特性，将成为了解选择性抑制CNS中mGlu2的生物学意义的有用工具。

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